September 2022 "Adhesion G protein-coupled receptors (aGPCRs) are cell-surface proteins with large extracellular regions that bind to multiple ligands to regulate key biological functions including neurodevelopment Modulating a single function of a specific aGPCR isoform while affecting no other function and no other receptor Here, we engineered an antibody, termed LK30, that binds to the extracellular region of the aGPCR ADGRL3 The LK30/ADGRL3 complex structure revealed that the LK30 binding site on ADGRL3 overlaps with the binding

It has begun to play important roles in drug development for complex diseases such as cancer, including macrophage heterogeneity in the tumor microenvironment while maintaining its predictive power of the trial results Despite its high mechanistic complexity, the modularized QSP platform can be readily reproduced, expanded Read more at the source #DrGPCR #GPCR #IndustryNews

critical for any higher organism, as it allows for prioritizing of vital information, preparation of responses The paraventricular nucleus of the thalamus (PVT) has recently been identified as an integrator of stimulus salience but the neurochemical basis and afferent input regarding salience signaling have remained elusive , including aversive, neutral and reinforcing sensory input. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "Background G protein-coupled receptor (GPCR) is the most targeted protein family by Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "Chemerin is the product of the RARRES2 gene which is secreted as a precursor of 143 Chemerin can signal via two G protein-coupled receptors, chem1 and chem2, as well as be bound to a third non-signaling receptor, CCRL2. role of different proteases in regulating the activation and inactivation of chemerin. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "For decades, glioblastoma multiforme (GBM), a type of the most lethal brain tumor, has remained Recently, many novel discoveries have underlined the regulatory roles of neurotransmitters in the microenvironment By targeting the receptors synaptically or non-synaptically, neurotransmitters activate multiple signaling GBM growth and development, requiring further research. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "Metabotropic γ-aminobutyric acid receptor (GABABR), a class C G protein-coupled receptor (GPCR) heterodimer, plays a crucial role in the central nervous system. Cryo-electron microscopy studies revealed a drastic conformational change upon activation and a unique deeper insertion of the α5 helix that causes the Gα subunit to open, releasing GDP, and forming the Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "Platelets are well characterized for their indispensable role in primary hemostasis to Research over the past years has provided a substantial body of evidence demonstrating that platelets The surface expression of pattern recognition receptors, such as TLR2 and TLR4, provides platelets with Platelet α-granules contain microbicidal proteins, chemokines and growth factors, which upon release Read more at the source #DrGPCR #GPCR #IndustryNews

ancestor of the mammalian membrane adenylyl cyclases " Mycobacterium tuberculosis adenylyl cyclase (AC) Rv1625c (TM) regions remains unknown. Here, we describe the cryo-EM structure of Cya bound to a stabilizing nanobody at 3.6 Å resolution. of catalytic activity in response to extracellular ligands." Read more at the source #DrGPCR #GPCR #IndustryNews

of salivary adenoid cystic carcinoma via the PI3K/AKT signaling pathway "Background CC chemokine receptor 9 (CCR9), an organ-specific chemokine receptor, interacts with its exclusive ligand CCL25 to promote However, the effect of CCR9 on salivary adenoid cystic carcinoma (SACC) malignant behavior remains unknown Methods Immunohistochemistry staining and RT–qPCR analyses were performed to detect the correlation Read more at the source #DrGPCR #GPCR #IndustryNews

💡Trainees are invited to participate by presenting a trainee talk, a poster, or a pre-recorded talk

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December 2021 "3-part randomized, double-blind, placebo-controlled Phase 1 study will evaluate TRV045 system (CNS) disorders, today announced it is advancing TRV045 into clinical development, following receipt TRV045 is the Company’s novel S1P1 receptor modulator being developed as a potential treatment for diabetic Read more at the source #DrGPCR #GPCR #IndustryNews

December 2021 " Dame Carol Robinson DBE, FRS, FRSC, FMedSci, Oxford University’s first female Professor of Chemistry, former president of the Royal Society of Chemistry and Founder of (and ongoing consultant Read more at the source #DrGPCR #GPCR #IndustryNews

Neurocrine Biosciences ”) announced 22 November 2021, the applicable waiting period under the Hart-Scott-Rodino Biosciences has agreed to pay Sosei Heptares an upfront payment of US$100 million, with the amount to be recognized as revenue in the fourth quarter of the financial year ending December 31, 2021." Read more at the source #DrGPCR #GPCR #IndustryNews

January 2022 "G-protein-coupled receptors’ star has been on the rise in biotech in recent years as researchers have discovered the vast potential for GPCR-targeting drugs in treating a range of health conditions Among those hitching their wagons to that star are Verily and Sosei Heptares , which have struck a research The financial details of the strategic collaboration weren’t released, but Sosei Heptares ’ past two Read more at the source #DrGPCR #GPCR #IndustryNews

Simply put, it represents what we do and why we do it. Read more at the source #DrGPCR #GPCR #IndustryNews

announced that TAVNEOS® (avacopan) has been approved within the European Union in combination with a rituximab or cyclophosphamide regimen for the treatment of adult patients with severe, active granulomatosis polyangiitis TAVNEOS will receive marketing authorization in all member states of the European Union, as well as in Read more at the source #DrGPCR #GPCR #IndustryNews

Under the joint research plan, the Danish giant will work with EraCal to identify novel drug targets relevant for food intake regulation and additional metabolic phenotypes. Although specific details of the collaboration are yet to be released, EraCal has confirmed that the Re ad more at the source #DrGPCR #GPCR #IndustryNews

co-founder "J an 27, 2022 07:00am Septerna wants to spark a second golden age in G-protein-coupled receptor Better known as GPCR, the fruitful research space has led to more than 700 approved drugs over previous decades—but the two-year-old biotech believes the area is still ripe for development, and it now has The company's co-founder, GPCR pioneer and Nobel laureate Robert Lefkowitz , M.D., has 50 years of experience Read more at the source #DrGPCR #GPCR #IndustryNews

the prediction of first-in-class small molecule agonists for a challenging orphan GPCR for a highly relevant systemsbiology #drugdiscovery #gpcr #deeptech #orphandrugs #pharma #partnerships #AI4drugdiscovery" Read

leaders in GPCRs pharmacology, immunology, drug discovery and development for auto-immune diseases" Read

clinical-stage global biopharmaceutical company developing novel oral therapeutics to treat a wide range Read more at the source #DrGPCR #GPCR #IndustryNews

de Montréal (Québec, Canada; “UdM”), to discover novel small molecules targeting G-Protein Coupled Receptors Read more at the source #DrGPCR #GPCR #IndustryNews

#ai #drugdiscovery #gpcr" Read more at the source #DrGPCR #GPCR #IndustryNews

January 2022 "Voltaire argued, “Perfection is attained by slow degrees; it requires the hand of time He might reverse himself and declare that the perfect can in fact be the friend of the good. screening, drug efficacy analyses, and toxicity studies; technologies that stabilize G protein–coupled receptors Read more at the source #DrGPCR #GPCR #IndustryNews

This award recognizes the combination of Steyaert’s fundamental research and his ability to apply the research to the development of therapeutic technologies. Steyaert bridged fundamental high-impact research in biomedical sciences with the mechanistic understanding Read more at the source #DrGPCR #GPCR #IndustryNews